Alpha-mangostin(AMG),a natural xanthone extracted from Garcinia mangostana Linn,has a variety of pharmacological therapeutic effects such as antioxidant activity,antibacterial activity,anticancer,and anti-inflammatory...Alpha-mangostin(AMG),a natural xanthone extracted from Garcinia mangostana Linn,has a variety of pharmacological therapeutic effects such as antioxidant activity,antibacterial activity,anticancer,and anti-inflammatory[1].However,it has poor aqueous-solubility and dissolution,which results in low bioavailability.Solid self-emulsifying drug delivery system(solid-SEDDS),an effective pharmaceutical strategy,offers the potential for enhancing the oral bioavailability of poorly water-soluble drugs[2].Therefore,solid-SEDDS is of interest as a potential method for enhancing the solubility and dissolution of AMG.展开更多
Objective:To investigate the antibiofilm activity of alphamangostin(AMG)loaded nanoparticle(nano AMG)against dental caries pathogen Streptococcus mutans.Methods:AMG was isolated from the peels of Garcinia mangostana L...Objective:To investigate the antibiofilm activity of alphamangostin(AMG)loaded nanoparticle(nano AMG)against dental caries pathogen Streptococcus mutans.Methods:AMG was isolated from the peels of Garcinia mangostana L.using silica gel columns and chemically analysed by high performance liquid chromatography and nuclear magnetic resonance.Nano AMG was prepared using the solvent evaporation method combined with high-speed homogenization.The nanoparticles were characterized using dynamic light scattering,field emission scanning electron microscopy(FE-SEM)and Fourier transform infrared spectroscopy(FTIR).The toxicity of nano AMG in fibroblast NIH/3 T3 cell line was determined using MTT method.The antibiofilm effect of nano AMG was determined through the evaluation of biofilm formation by Streptococcus mutans using a 96-well plate.Biofilm biomass was quantified using crystal violet.Cell viability was observed under confocal microscopy using LIVE/DEAD Bac Light staining.Moreover,gene expression was determined by quantitative real-time PCR and membrane permeabilization activity by measuring the uptake of o-nitrophenol-β-D-galactoside.Results:Nano AMG size was in a range of 10-50 nm with a polydispersity index of<0.3 and zeta potential value of-35.2 m V.The size and the incorporation of AMG in the nanoparticles were confirmed by FE-SEM and FTIR analyses.The IC50 values of the test agents on NIH/3 T3 cells were(9.80±0.63)μg/m L for AMG and(8.70±0.81)μg/m L for nano AMG,while no toxicity was generated from excipients used to prepare nanoparticles.In the early stage of biofilm formation,treatment with 6.25μmol/L nano AMG caused a reduction in biofilm biomass up to 49.1%,compared to 33.4%for AMG.In contrast,biofilms at the late stage were more resistant to the test agents.At 96μmol/L(=10×MIC),nano AMG reduced only 20.7%of biofilm biomass while AMG did not showany effect.Expressions of gtf B and gtf C genes involved in biofilm formation were down-regulated 3.3 and 12.5 folds,respectively,compared to AMG(2.4 and 7.6 folds,respectively).LIVE/DEAD Bac Light fluorescence staining and microscopy observation indicated that biofilm cells were killed by both nano AMG and AMG at 48μmol/L(=5×MIC).In addition,membrane permeabilization activity was increased in a time dependent manner and higher in nano AMG treated cells compared to AMG.Conclusions:AMG coated nanoparticle can enhance AMG bioactivity and can be used as a new and promising antibiofilm agent.展开更多
The effects of drying temperature and extraction methods on α-mangostin content in mangosteen pericarp （Garcinia mangostana L.） powder were investigated. In the first part of experiment suitable drying temperature ...The effects of drying temperature and extraction methods on α-mangostin content in mangosteen pericarp （Garcinia mangostana L.） powder were investigated. In the first part of experiment suitable drying temperature for retention α-mangostin content was determined. Three levels of drying temperatures （55, 65 and 75 ℃） were used in this study. The drying rates were increased with drying temperature. Room temperature extraction method was performed to investigate the effect of drying temperature on retention α-mangostin content in mangosteen pericarp. The α-mangostin content extracted at three different drying temperatures （55, 65 and 75 ℃） was 35.98 ± 0.49%, 40.32 ± 0.24%, and 37.79±0.34% w/w, respectively. The results showed that the suitable temperature for drying mangosteen pericarp was 65 ℃ that gave the highest of α-mangostin content. The second part of experiment was the comparison between extraction methods, such as shaking water bath extraction （SWE）, soxhlet extraction （SE） and microwave-assisted extraction （MAE）. The results show that MAE gave the highest extraction rate and α-mangostin content as compare to SWE and SE. The α-mangostin content extraction from SWE, SE and MAE are 45.83 ± 0.02, 34.82± 0.17 and 49.79 ± 0.15% w/w of crude extract, respectively.展开更多
文摘Alpha-mangostin(AMG),a natural xanthone extracted from Garcinia mangostana Linn,has a variety of pharmacological therapeutic effects such as antioxidant activity,antibacterial activity,anticancer,and anti-inflammatory[1].However,it has poor aqueous-solubility and dissolution,which results in low bioavailability.Solid self-emulsifying drug delivery system(solid-SEDDS),an effective pharmaceutical strategy,offers the potential for enhancing the oral bioavailability of poorly water-soluble drugs[2].Therefore,solid-SEDDS is of interest as a potential method for enhancing the solubility and dissolution of AMG.
基金supported by the NAFOSTED research grant 106-NN.02-2016.19 to Phuong T.M.Nguyen.
文摘Objective:To investigate the antibiofilm activity of alphamangostin(AMG)loaded nanoparticle(nano AMG)against dental caries pathogen Streptococcus mutans.Methods:AMG was isolated from the peels of Garcinia mangostana L.using silica gel columns and chemically analysed by high performance liquid chromatography and nuclear magnetic resonance.Nano AMG was prepared using the solvent evaporation method combined with high-speed homogenization.The nanoparticles were characterized using dynamic light scattering,field emission scanning electron microscopy(FE-SEM)and Fourier transform infrared spectroscopy(FTIR).The toxicity of nano AMG in fibroblast NIH/3 T3 cell line was determined using MTT method.The antibiofilm effect of nano AMG was determined through the evaluation of biofilm formation by Streptococcus mutans using a 96-well plate.Biofilm biomass was quantified using crystal violet.Cell viability was observed under confocal microscopy using LIVE/DEAD Bac Light staining.Moreover,gene expression was determined by quantitative real-time PCR and membrane permeabilization activity by measuring the uptake of o-nitrophenol-β-D-galactoside.Results:Nano AMG size was in a range of 10-50 nm with a polydispersity index of<0.3 and zeta potential value of-35.2 m V.The size and the incorporation of AMG in the nanoparticles were confirmed by FE-SEM and FTIR analyses.The IC50 values of the test agents on NIH/3 T3 cells were(9.80±0.63)μg/m L for AMG and(8.70±0.81)μg/m L for nano AMG,while no toxicity was generated from excipients used to prepare nanoparticles.In the early stage of biofilm formation,treatment with 6.25μmol/L nano AMG caused a reduction in biofilm biomass up to 49.1%,compared to 33.4%for AMG.In contrast,biofilms at the late stage were more resistant to the test agents.At 96μmol/L(=10×MIC),nano AMG reduced only 20.7%of biofilm biomass while AMG did not showany effect.Expressions of gtf B and gtf C genes involved in biofilm formation were down-regulated 3.3 and 12.5 folds,respectively,compared to AMG(2.4 and 7.6 folds,respectively).LIVE/DEAD Bac Light fluorescence staining and microscopy observation indicated that biofilm cells were killed by both nano AMG and AMG at 48μmol/L(=5×MIC).In addition,membrane permeabilization activity was increased in a time dependent manner and higher in nano AMG treated cells compared to AMG.Conclusions:AMG coated nanoparticle can enhance AMG bioactivity and can be used as a new and promising antibiofilm agent.
文摘The effects of drying temperature and extraction methods on α-mangostin content in mangosteen pericarp （Garcinia mangostana L.） powder were investigated. In the first part of experiment suitable drying temperature for retention α-mangostin content was determined. Three levels of drying temperatures （55, 65 and 75 ℃） were used in this study. The drying rates were increased with drying temperature. Room temperature extraction method was performed to investigate the effect of drying temperature on retention α-mangostin content in mangosteen pericarp. The α-mangostin content extracted at three different drying temperatures （55, 65 and 75 ℃） was 35.98 ± 0.49%, 40.32 ± 0.24%, and 37.79±0.34% w/w, respectively. The results showed that the suitable temperature for drying mangosteen pericarp was 65 ℃ that gave the highest of α-mangostin content. The second part of experiment was the comparison between extraction methods, such as shaking water bath extraction （SWE）, soxhlet extraction （SE） and microwave-assisted extraction （MAE）. The results show that MAE gave the highest extraction rate and α-mangostin content as compare to SWE and SE. The α-mangostin content extraction from SWE, SE and MAE are 45.83 ± 0.02, 34.82± 0.17 and 49.79 ± 0.15% w/w of crude extract, respectively.
